Thiazole–driven heterocyclic hybrids as EGFR inhibitors: progress in synthesis and anticancer applications

Abstract

Despite considerable progress in therapeutic developments, cancer still stands as one of the most common and lethal health challenges worldwide. Targeting the EGFR signaling pathway has emerged as a key approach in cancer therapy. Inhibiting the intracellular tyrosine kinase domain of EGFR has demonstrated significant therapeutic benefits. To discover effective EGFR tyrosine kinase inhibitors (TKIs), numerous small molecules, particularly thiazole-based hybrids have been developed using molecular modelling techniques. However, challenges such as epigenetic mutations and acquired resistance have limited their long-term efficacy, highlighting the need for continued research in this area. Recent efforts have focused on understanding genetic alterations within the EGFR tyrosine kinase domain, paving the way for the development of more selective and potent inhibitors. This review presents an overview of the role and current landscape of EGFR inhibitors in cancer treatment, with a particular emphasis on recent progress in the design, synthesis, and development of novel thiazole hybrid compounds as promising selective EGFR TKIs.